A Clinically Relevant Androgen Receptor Mutation Confers Resistance to Second-Generation Antiandrogens Enzalutamide and ARN-509
Citations
2,221 citations
1,055 citations
980 citations
926 citations
803 citations
Cites background from "A Clinically Relevant Androgen Rece..."
...This ARmutation has also been recovered from patients with resistance to ARN-509 but only in a minority of cases (Joseph et al., 2013)....
[...]
...For example, one of these low GR tumors contained the F876L AR mutation that converts both ARN-509 and enzalutamide to agonists and is associated with clinical resistance (Balbas et al., 2013; Joseph et al., 2013; Korpal et al., 2013)....
[...]
...We and others have recently identified an AR point mutation as one resistancemechanism by derivation of drug-resistant sublines following prolonged exposure to enzalutamide or ARN-509 (Balbas et al., 2013; Joseph et al., 2013; Korpal et al., 2013)....
[...]
...…androgen-deprivation therapy or abiraterone by simply elevating AR levels, whereas the increased selection pressure conferred by second-generation antiandrogens requires an alternative strategy such as GR bypass or AR mutation (Balbas et al., 2013; Joseph et al., 2013; Korpal et al., 2013)....
[...]
References
12,583 citations
3,866 citations
3,132 citations
2,320 citations
2,141 citations